Eye drops, broad spectrum bactericidal antibiotic (gyrase inhibitor)
Each ml contains:
Active ingredient: lomefloxacin 3 mg (as hydrochloride 3.31 mg)
Excipients: glycerol 26mg, disodium edetate 0.1 mg, sodium hydroxide I N q.s., water for injection to 1 ml
Preservative: benzalkonium chloride O.02 mg
Lomefloxacin, a diftuorinated quinoione derivative, is a bacterial gyrase inhibitor. It is effective against a broad spectrum of gram positive and gram negative bacteria. The acute toxicity of lomefloxacin following systemic and topical ophthalmic application is low. Lomefloxacin interferes with bacterial DNA related processes like initiation, elongation, and termination phases of replication, transcription, DNA repair, recombination, transposition supercciling and relaxation of DNA. The target molecule for quinolones is the A subunit of bacterial enzyme gyrase (topoisomerase ll). The forming of a stable complex between the quinolone and the whole gyrase tetramer A2B2 leads to impaired enzyme functions, resulting in a rapid killing of sensitive bacteria. Plasmid-mediated transfer of
resistance has not been observed so far. The frequency of development of resistance through spontaneous mutations is less than 10-8 to 10-9 which is similar to other quinolones Cross- resistance has only been reported with other quinolones. But not with any other group of antibiotics. No clinical studies are available about the efficacy in cases of infections with Chlamydia.
The antimicrobial spectrum of Lomeftoxacin is as follows :
The antimicrobial spectrum includes gram-positive and gram negative bacteria, as reported from various in-vitro studies.
A meta-analysis based on phase 11 and phase 1Il clinic studies revealed the following sensitive germs. Sensitive germs (MIC90 -c 4 ug/ml)
Gram-positive: Staph. epidermidis, Staph. aureus, Bacillus, Corynebacterium.
Gram-negative: Branhamella catarrbalis, Neisseria sp., Enterobacter spp., Haemophilus influenza, Klebsiella, Moraxella,
Proteus, Pseudomonas aeruginosa, Pseudomonas spp., Serratia spp., Acinetobacter spp., Alcaligenes faecalis , Flavobacterium spp. Anaerobic: Propionibacterium acnes. Intermediate sensitive germs (MIC90 = 4-16 J.1g1ml)
Gram-positive: Streptococcus pneumoniae, streptococcus spp., Micrococcus, Enterococcus faecialis. Resistant genns (MIC90 > 16 J.1g1ml) Clostridium difficile, Mycobacterium.
In rabbits, topical application of 50 I of a solution containin 0.3% Cl4_labelled lomefloxecin revealed the following results:
cornea 55.68 ug-eq/g 15 minutes conjunctiva 11.39 ug-eq/g 15 minutes aqueous humour 7.58 ug-eq/g 60 minutes
In animal studies, the tear concentration after two installations of 50 III 0.3% Lomeffoxecin was 7-27 J.1g1ml at 6 hours. And more than 3 ~glml even at 24 hours were observed. Although these results can not directly be transferred to the human eye since physiology of the cornea and penetration through the cornea vary considerably between rabbits and humans, penetration of lomefloxacin through the human cornea has been confirmed. In humans, concentrations of
1.3-2.7 J.1g1ml in the anterior chamber have been found 90-180 min after topical application. This concentration, however,may not be high enough for the treatment of endophthalmitis. Systemic absorption following topical instillation of 0.3% Lomefloxacin eye drops is very low. After application of four times daily 2 drops during two weeks, blood levels were below the detection limit of 0.005 J.1g1ml.
Bacterial infections of the anterior segment including conjunctivitis, blepharitis, and blepharo-conjunctivitis which are due to lomctloxacin susceptible gems.
Adults& children (above I year of age): Instill one drop 2-3 times daily. At the beginning of treatment, applications should be more frequent: apply 5 drops within 20 minutes or I drop every hour during 6-10 hours. Duration of treatment is 7 to 9 days.
Restriction on use :
Hypersensitivity to the active ingredient (Lomefloxacin), to excipients, or to quinolones in general. In animal studies arthrotoxicity in juvenile rats was reported at high (300mg/kg) but not at low (< 100 mg/kg) dosages.topical application, even with complete absorption, lead to a total dosage of only 2mglday. The maximum daily dose per kg is therefore in the range of about 20-50 ug/kg which is several orders of magnitude below the arthrotoxic threshold. No adverse effects were noted in children included in clinical studies, although these data are limited.
Long term treatment with antibiotics may enhance development of secondary fungal infections or the growth of resistant bacteria. Some isolated cases of phototoxicity have been reported after systemic but not after topical ophthalmic use oflomefloxcin. Nevertheless, during treatment with orchacin intensive exposure to sunlight or UV-
radiation should be avoided.
Pregnancy and lactation :
After high systemic doses of Lcmefloxacin (50-100 mg/kg), variation of caudal vertebrae have been observed in rabbit foetus. Systemic Lomefloxacin passes the Placental barrier and is also excreted in the maternal milk. Clinical Studies on the use of Lomefloxacin eye drops during human pregnancy or lactation are not available. Therefore, Lomeffoxacin should not be used when the potential benefit to the pregnant I lactating woman out-weighs the
potential risk to the foetus or infant. Pregnancy category: C
Adverse reaction :
Slight and transient burning immediately after instillation of the eye drops has been occasionally reported in 4.7% of users. Although phototoxicity has not been reported after ophthalmic use, photosensitization is possible. Since the following allergic reactions have been reported after systemic use of lomefloxacin, they cannot be excluded after topical ophthalmic use: allergic reactions, asthma, dyspnoea, urticaria, erythema, pruritis, and hypersensitization.
in order 10 avoid reduction of efficacy, no ophthalmic preparations containing heavy metals.sucb as zinc, should be used duringl5 minutes preceding and following application of orchacin.
Bacteriostatic ophthalmic antibiotics should not be used concomitantly with Orchacin eye drops. Other interactions
have not been described to date.
There is no risk of diverse effects due to accidental oral ingestion since one bottle of 5ml eye drop solution contains only 15mg Lomefloxacin. This corresponds to 3.75% of the recommended oral daily dose for adults of400 mg lomefloxacin.in case of systemic ingestion irrigation of the stomach may be appropriate in young children to decrease further absorption.
Note for patients wearing contact lenses:
Contact lenses should not be worn during ophthalmic infections. When two or more ophthalmic preparations are used concomitantly, an interval of at least 5 minutes should be observed between the medications, in order to avoid washing-out of the drug.
Orchacin eye drops may be used up to the date indicated with < EXP» on the pack. Close the bottle immediately after use. Store at room temperature ( <25°C ) and protected from light. Do not use
after I month from first opening. Keep out <?f the reach of children.
Dropper bottle of 5ml
Manufactured by :
Orchidia Pharmaceutical Industries